title: Biochemical screening assays to identify HIV-1 integrase inhibitors.
abstract: Human immunodeficiency virus type 1 (HIV-1) integrase is, in addition to reverse transcriptase and protease, an important enzymatic target for antiretroviral drug development. Integrase plays a critical role in the HIV-1 life cycle coordinating the integration of the reverse-transcribed viral DNA into the host genome. This integration step is the net result of two consecutive integrase-related processes. First, integrase removes a dinucleotide from the 3' viral DNA ends in a process called 3'-processing. Next, in a process called strand transfer, the viral DNA is integrated into the host genomic DNA. Early on, biochemical assays have played a critical role in understanding the function of HIV-1 integrase and the discovery of small-molecule inhibitors. In this chapter we describe two biochemical assays to identify inhibitors of the 3'-processing and strand transfer process of HIV-1 integrase.
authors.affiliation: Janssen Infectious Diseases-Diagnostics BVBA, Johnson & Johnson Corporation, Beerse, Belgium.
authors.forename: Marleen
authors.initials: M
authors.lastname: Clynhens
authors.forename: Alexandra
authors.initials: A
authors.lastname: Smets
authors.forename: Inge
authors.initials: I
authors.lastname: Vereycken
authors.forename: Marnix
authors.initials: M
authors.lastname: Van Loock
authors.forename: Reginald
authors.initials: R
authors.lastname: Clayton
authors.forename: Geert
authors.initials: G
authors.lastname: Meersseman
authors.forename: Olivia
authors.initials: O
authors.lastname: Goethals
mesh_terms: D004279:DNA, Viral / Q000235:genetics / Q000378:metabolism; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology* / Q000235:genetics; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D016662:Virus Integration / Q000187:drug effects
chemical_list: D004279:DNA, Viral; D019428:HIV Integrase Inhibitors; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1